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CL2016001876A1 - Macrociclos de diarilo como moduladores de la proteína quinasa - Google Patents

Macrociclos de diarilo como moduladores de la proteína quinasa

Info

Publication number
CL2016001876A1
CL2016001876A1 CL2016001876A CL2016001876A CL2016001876A1 CL 2016001876 A1 CL2016001876 A1 CL 2016001876A1 CL 2016001876 A CL2016001876 A CL 2016001876A CL 2016001876 A CL2016001876 A CL 2016001876A CL 2016001876 A1 CL2016001876 A1 CL 2016001876A1
Authority
CL
Chile
Prior art keywords
protein kinase
kinase modulators
macrocycles
diaryl
diaryl macrocycles
Prior art date
Application number
CL2016001876A
Other languages
English (en)
Spanish (es)
Inventor
Dayong Zhai
Jingrong Jean Cui
Yishan Li
Evan W Rogers
Original Assignee
Tp Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tp Therapeutics Inc filed Critical Tp Therapeutics Inc
Publication of CL2016001876A1 publication Critical patent/CL2016001876A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
CL2016001876A 2014-01-24 2016-07-22 Macrociclos de diarilo como moduladores de la proteína quinasa CL2016001876A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461931506P 2014-01-24 2014-01-24
US201462049326P 2014-09-11 2014-09-11
US201562106301P 2015-01-22 2015-01-22

Publications (1)

Publication Number Publication Date
CL2016001876A1 true CL2016001876A1 (es) 2017-02-03

Family

ID=53682127

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2016001876A CL2016001876A1 (es) 2014-01-24 2016-07-22 Macrociclos de diarilo como moduladores de la proteína quinasa

Country Status (34)

Country Link
US (6) US9714258B2 (he)
EP (6) EP3636650A1 (he)
JP (5) JP6490713B2 (he)
KR (1) KR102402179B1 (he)
CN (3) CN106170289B (he)
AP (1) AP2016009383A0 (he)
AU (2) AU2015209239B2 (he)
CA (1) CA2936079C (he)
CL (1) CL2016001876A1 (he)
CY (1) CY1121850T1 (he)
DK (3) DK3097107T3 (he)
EA (2) EA201892241A1 (he)
ES (3) ES2976459T3 (he)
FI (2) FI3636649T3 (he)
HK (1) HK1231407A1 (he)
HR (3) HRP20240503T1 (he)
HU (3) HUE066590T2 (he)
IL (2) IL246860B (he)
LT (3) LT3097107T (he)
MX (2) MX392904B (he)
MY (1) MY193524A (he)
NO (1) NO2025015I1 (he)
NZ (2) NZ761094A (he)
PE (1) PE20160931A1 (he)
PH (1) PH12016501463A1 (he)
PL (3) PL3572416T3 (he)
PT (3) PT3572416T (he)
RS (3) RS59059B1 (he)
SG (2) SG11201605929RA (he)
SI (3) SI3572416T1 (he)
SM (3) SMT202300008T1 (he)
UA (1) UA121206C2 (he)
WO (1) WO2015112806A2 (he)
ZA (2) ZA201604654B (he)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103965200B (zh) 2008-09-22 2016-06-08 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物
ES2588504T3 (es) 2008-10-22 2016-11-03 Array Biopharma, Inc. Compuestos de pirazolo[1,5-a]pirimidina sustituidos como compuestos intermedios en la síntesis de inhibidores de TRK quinasa
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
RU2594742C2 (ru) 2010-05-20 2016-08-20 Эррэй Биофарма Инк. Макроциклические соединения в качестве ингибиторов киназы trk
PT3572416T (pt) * 2014-01-24 2022-12-06 Turning Point Therapeutics Inc Macrociclos de diarilo como moduladores de roteínacinases
CA2967951C (en) 2014-11-16 2023-11-07 Array Biopharma, Inc. Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
US10758525B2 (en) 2015-01-22 2020-09-01 MyoKardia, Inc. 4-methylsulfonyl-substituted piperidine urea compounds
MA41667A1 (fr) 2015-06-01 2018-08-31 Loxo Oncology Inc Procede de diagnostic et de traitement du cancer
CA2989327A1 (en) * 2015-07-02 2017-01-05 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
DK3319969T3 (da) * 2015-07-06 2024-07-08 Turning Point Therapeutics Inc Diaryl-makrocyklus-polymorf
EP3322706B1 (en) 2015-07-16 2020-11-11 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
CN108026109B (zh) * 2015-07-21 2021-03-02 特普医药公司 手性二芳基大环及其用途
SG11201803438XA (en) 2015-10-26 2018-05-30 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US11278521B2 (en) 2015-12-15 2022-03-22 University Of South Florida GAS5 binding compounds, formulations, and uses thereof
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
BR112018070017A2 (pt) 2016-04-04 2019-02-05 Loxo Oncology Inc métodos de tratamento de cânceres pediátricos
DK3439662T3 (da) 2016-04-04 2024-09-02 Loxo Oncology Inc Væskeformige formuleringer af (s)-n-(5-((r)-2-(2,5-difluorphenyl)-pyrrolidin-1-yl)-pyrazol[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid
DK3800189T3 (da) 2016-05-18 2023-07-31 Loxo Oncology Inc Fremstilling af (s)-n-(5-((r)-2-(2,5-difluorphenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid
TW201815799A (zh) * 2016-07-28 2018-05-01 美商Ｔｐ生物醫藥公司 巨環激酶抑制劑
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
WO2018136661A1 (en) 2017-01-18 2018-07-26 Andrews Steven W SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
TWI808958B (zh) * 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CN107586796B (zh) * 2017-07-20 2021-08-06 暨明医药科技（苏州）有限公司 (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法
SI3658148T1 (sl) * 2017-07-28 2024-10-30 Turning Point Therapeutics, Inc. Makrociklične spojine in njihova uporaba
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
CA3080157A1 (en) 2017-10-26 2019-05-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
CN109516999B (zh) * 2017-11-01 2021-08-17 郑州泰基鸿诺医药股份有限公司 用作蛋白质激酶调节剂的化合物及其应用
TW201927790A (zh) * 2017-11-10 2019-07-16 美商安捷克斯製藥公司 作為trk激酶抑制劑之巨環化合物及其用途
BR112020012319A2 (pt) 2017-12-19 2020-11-24 Turning Point Therapeutics, Inc. compostos macrocíclicos para tratar doença
US20210087206A1 (en) 2017-12-19 2021-03-25 Turning Point Therapeutics, Inc. Macrocyclic kinase inhibitors and their use
JP7150356B2 (ja) * 2017-12-22 2022-10-11 深▲チェン▼市塔吉瑞生物医薬有限公司 置換ピラゾロ［１，５－ａ］ピリミジン化合物並びにその医薬組成物および使用
CA3087354C (en) 2018-01-18 2023-01-03 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
EP3740486A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
TW201938169A (zh) 2018-01-18 2019-10-01 美商亞雷生物製藥股份有限公司 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物
EP3744723B1 (en) * 2018-01-23 2023-10-18 Shenzhen TargetRx, Inc. Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound
CN111511749B (zh) * 2018-01-30 2022-02-08 上海吉倍生物技术有限公司 具有大环分子结构的化合物及其用途
CN110156813B (zh) * 2018-02-13 2023-07-25 北京诺诚健华医药科技有限公司 作为trk抑制剂的杂环化合物
BR112020019399A2 (pt) * 2018-03-28 2021-01-05 Fochon Pharmaceuticals, Ltd. Compostos macrocíclicos como inibidores de trk quinases
US20210023086A1 (en) 2018-03-29 2021-01-28 Loxo Oncology, Inc. Treatment of trk-associated cancers
US11358973B2 (en) 2018-04-16 2022-06-14 Shenzhen Targetrx, Inc. Di(hetero)aryl macrocyclic compound for inhibiting protein kinase activity
PL3786167T3 (pl) * 2018-04-25 2024-11-25 Primegene (Beijing) Co., Ltd. Diarylowy związek makrocykliczny i kompozycja farmaceutyczna oraz ich zastosowanie
CN111918868B (zh) * 2018-05-04 2022-12-30 正大天晴药业集团股份有限公司 作为蛋白激酶调节剂的二芳基大环化合物
CN110627812B (zh) 2018-06-25 2022-10-11 北京诺诚健华医药科技有限公司 作为trk抑制剂的杂环化合物
CA3224945A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET
CN110950889B (zh) * 2018-09-27 2022-04-05 北京赛林泰医药技术有限公司 一种多靶点激酶抑制剂及其制备方法和用途
CN112955453B (zh) * 2018-09-29 2022-04-19 山东绿叶制药有限公司 作为选择性Trk抑制剂的吡唑并嘧啶衍生物
AU2019364336B2 (en) 2018-10-22 2023-11-16 Alumis Inc. TYK2 inhibitors and uses thereof
CN111171049B (zh) * 2018-11-09 2021-06-04 山东轩竹医药科技有限公司 酪氨酸激酶抑制剂及其用途
SG11202104609SA (en) * 2018-11-09 2021-06-29 Shandong Xuanzhu Pharma Co Ltd Macrocyclic tyrosine kinase inhibitor and uses thereof
AU2019385397A1 (en) * 2018-11-19 2021-04-22 Dana-Farber Cancer Institute, Inc. Macrocyclic inhibitors of DYRK1A
JP2022515198A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
CN111592541B (zh) * 2019-02-21 2021-09-10 山东轩竹医药科技有限公司 大环类激酶抑制剂及其用途
JP7586829B2 (ja) * 2019-03-11 2024-11-19 アルミス インコーポレイテッド Ｔｙｋ２阻害剤およびその使用
CA3134814A1 (en) 2019-03-26 2020-10-01 Ventyx Biosciences, Inc. Tyk2 pseudokinase ligands
CN113727984B (zh) * 2019-05-21 2024-03-15 浙江海正药业股份有限公司 大环类衍生物、及其制备方法和用途
WO2020257165A1 (en) * 2019-06-19 2020-12-24 Turning Point Therapeutics, Inc. Macrocycles for use in treating disease
WO2020257189A1 (en) * 2019-06-19 2020-12-24 Turning Point Therapeutics, Inc. Macrocycles for treating disease
CA3143043A1 (en) * 2019-06-19 2020-12-24 Turning Point Therapeutics, Inc. Polymorphs of a macrocyclic kinase inhibitor
JP7617861B2 (ja) * 2019-06-21 2025-01-20 ヤンセン ファーマシューティカ エヌ．ベー． Ｍｃｌ－１の大環状阻害剤
CN113773335B (zh) * 2019-06-21 2024-12-03 成都海博为药业有限公司 一种作为蛋白质激酶抑制剂的化合物及其制备方法和用途
WO2021027503A1 (zh) * 2019-08-12 2021-02-18 罗欣药业(上海)有限公司 三环类化合物、其制备方法、中间体及应用
WO2021063276A1 (zh) * 2019-09-30 2021-04-08 浙江海正药业股份有限公司 大环类衍生物及其制备方法和用途
JP2023504046A (ja) 2019-11-27 2023-02-01 ターニング・ポイント・セラピューティクス・インコーポレイテッド ジアリール大環状化合物を含む併用療法
MX2022006500A (es) 2019-11-27 2022-07-04 Turning Point Therapeutics Inc Terapia de combinacion que involucra compuestos macrociclicos de diarilo.
ES2987981T3 (es) 2019-12-03 2024-11-19 Turning Point Therapeutics Inc Macrociclos para uso en el tratamiento de enfermedades
US20230101747A1 (en) 2019-12-06 2023-03-30 Schrödinger, Inc. Cyclic compounds and methods of using same
CN113045587A (zh) * 2019-12-27 2021-06-29 成都倍特药业股份有限公司 一种大环结构化合物的晶型及其制备方法
MX2022007171A (es) 2019-12-27 2022-08-22 Schroedinger Inc Compuestos cíclicos y métodos de uso de estos.
CN113135938B (zh) * 2020-01-19 2022-06-14 山东轩竹医药科技有限公司 取代的大环类酪氨酸激酶抑制剂及其用途
JP2023515687A (ja) * 2020-03-02 2023-04-13 ターニング・ポイント・セラピューティクス・インコーポレイテッド 大環状化合物の治療使用
PE20230609A1 (es) 2020-05-04 2023-04-13 Amgen Inc Compuestos heterociclicos como agonistas del receptor de activacion expresado en las celulas mieloides 2 y metodos de uso
US20230183265A1 (en) * 2020-05-08 2023-06-15 Shandong Xuanzhu Pharma Co., Ltd. Crystal Form of Macrocyclic Tyrosine Kinase Inhibitor and Preparation Method therefor
WO2021244609A1 (zh) * 2020-06-04 2021-12-09 成都倍特药业股份有限公司 具有大环结构的化合物及其用途
US20230257396A1 (en) * 2020-07-10 2023-08-17 Blossomhill Therapeutics, Inc. Macrocycles and their use
US20230365584A1 (en) 2020-09-10 2023-11-16 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
JP2024505890A (ja) 2021-01-26 2024-02-08 シュレーディンガー， インコーポレイテッド がん、自己免疫及び炎症性障害の治療に有用な三環式化合物
WO2022182845A1 (en) * 2021-02-25 2022-09-01 Blossomhill Therapeutics, Inc. Macrocycles and their use
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
CN116063326A (zh) * 2021-11-02 2023-05-05 赛诺哈勃药业（成都）有限公司 作为蛋白激酶调节剂的含氨基大环化合物
US20250074920A1 (en) * 2022-01-05 2025-03-06 Blossomhill Therapeutics, Inc. Macrocyclic compounds and use as kinase inhibitors
CN115746023B (zh) * 2022-10-27 2024-08-09 复旦大学 一种作为蛋白激酶抑制剂的含吲唑结构的杂环大环化合物及其制备方法
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4838925A (en) 1986-04-25 1989-06-13 E. I. Du Pont De Nemours And Company Heterocyclic acyl sulfonamides
ES2021105B3 (es) 1987-03-07 1991-10-16 Bayer Ag Procedimiento para la obtencion de 5-amino-4,6-dihalogeno piridinas.
EP0690843B1 (en) 1993-03-25 2000-08-30 PHARMACIA & UPJOHN COMPANY Formyl- or cyano- substituted indole derivatives having dopaminergic activity
FR2746309B1 (fr) 1996-03-22 1998-04-17 Oreal Composition de teinture des fibres keratiniques contenant des pyrazolopyrimidineoxo ; leur utilisation pour la teinture comme coupleurs, procedes de teinture
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
FR2793791B1 (fr) 1999-05-19 2002-01-25 Univ Paris 7 Denis Diderot Nouveaux composes inhibiteurs specifiques de phospholipases a2
ES2250459T3 (es) 2000-07-31 2006-04-16 F. Hoffmann-La Roche Ag Derivados de piperazina.
AU2002254114A1 (en) 2001-03-23 2002-10-08 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
EA201100450A1 (ru) * 2008-09-08 2011-10-31 Мерк Патент Гмбх Макроциклические пирамидины в качестве ингибиторов протеинкиназы
CN103965200B (zh) 2008-09-22 2016-06-08 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物
ES2588504T3 (es) 2008-10-22 2016-11-03 Array Biopharma, Inc. Compuestos de pirazolo[1,5-a]pirimidina sustituidos como compuestos intermedios en la síntesis de inhibidores de TRK quinasa
ES2545541T3 (es) 2008-10-31 2015-09-11 Genentech, Inc. Compuestos de pirazolopirimidina inhibidores de JAK y métodos
WO2010063487A1 (en) 2008-12-05 2010-06-10 Merz Pharma Gmbh & Co. Kgaa Pyrazolopyrimidines, a process for their preparation and their use as medicine
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US20110029480A1 (en) * 2009-08-03 2011-02-03 IntelliCubes, Inc. Method of Compiling Multiple Data Sources into One Dataset
EP2509979B1 (en) 2009-12-07 2016-05-25 Boehringer Ingelheim International GmbH Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
WO2011071716A1 (en) 2009-12-07 2011-06-16 Boehringer Ingelheim International Gmbh Heterocyclic compounds containing an indole core
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
RU2594742C2 (ru) 2010-05-20 2016-08-20 Эррэй Биофарма Инк. Макроциклические соединения в качестве ингибиторов киназы trk
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
WO2012075393A2 (en) 2010-12-02 2012-06-07 President And Fellows Of Harvard College Activators of proteasomal degradation and uses thereof
EP2508607A1 (en) * 2011-04-07 2012-10-10 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for liver regeneration and for treatment of liver failure
WO2013001310A1 (en) * 2011-06-30 2013-01-03 Centro Nacional De Investigaciones Oncológicas (Cnio) Macrocyclic compounds and their use as cdk8 inhibitors
AU2012299223A1 (en) * 2011-08-19 2014-02-27 Merck Sharp & Dohme Corp. Process and intermediates for preparing macrolactams
WO2013045702A2 (en) 2011-09-29 2013-04-04 L'oreal Dye composition comprising a non-glycosyl iridoid compound and a specific nucleophile or an amino or thio polymer, dyeing process, and device therefor
WO2013045701A2 (en) 2011-09-29 2013-04-04 L'oreal Dyeing process using a composition comprising a glycosyl iridoid compound and a nucleophile or an amino or thio polymer, composition and devices therefor
JP6046728B2 (ja) * 2011-09-30 2016-12-21 オンコデザイン エス．ア． 大環状ｆｌｔ３キナーゼ阻害剤
KR20140077963A (ko) 2011-10-20 2014-06-24 글락소스미스클라인 엘엘씨 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체
MX350844B (es) 2012-03-06 2017-09-22 Pfizer Derivados macrocíclicos para el tratamiento de enfermedades proliferativas.
MX345830B (es) 2012-03-09 2017-02-17 Lexicon Pharmaceuticals Inc Compuestos a base de pirazol[1,5-a]pirimidina, composiciones que los comprenden, y metodos para su uso.
NZ630719A (en) * 2012-03-09 2017-01-27 Lexicon Pharmaceuticals Inc Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
JP2016506921A (ja) 2013-01-30 2016-03-07 バイエル ファーマ アクチエンゲゼルシャフト アミノ置換イソチアゾール
EP2989082A1 (en) 2013-04-23 2016-03-02 LEK Pharmaceuticals d.d. Novel synthetic process to 8-chloro-1-methyl-benzo[d]azepine, novel intermediates and the production thereof
EP3026051A4 (en) 2013-07-24 2017-03-08 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2015073267A1 (en) 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
PT3572416T (pt) 2014-01-24 2022-12-06 Turning Point Therapeutics Inc Macrociclos de diarilo como moduladores de roteínacinases
WO2016070241A1 (en) 2014-11-03 2016-05-12 Ctxt Pty Ltd Triazine compounds, compositions and synthesis
RU2708674C2 (ru) 2014-12-15 2019-12-11 СиЭмДжи ФАРМАСЬЮТИКАЛ КО., ЛТД. Конденсированные кольцевые гетероарильные соединения и их применение в качестве ингибиторов trk
CN107531666A (zh) 2015-02-20 2018-01-02 里格尔药品股份有限公司 Gdf‑8抑制剂
EP3267996B1 (en) 2015-03-12 2020-11-11 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
WO2016144844A1 (en) 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Carboxamide inhibitors of irak4 activity
EA201792421A1 (ru) 2015-05-05 2018-05-31 Байер Фарма Акциенгезельшафт Амидозамещенные производные циклогексана
CA2989327A1 (en) 2015-07-02 2017-01-05 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
DK3319969T3 (da) 2015-07-06 2024-07-08 Turning Point Therapeutics Inc Diaryl-makrocyklus-polymorf
CN108026109B (zh) 2015-07-21 2021-03-02 特普医药公司 手性二芳基大环及其用途
SG11201803438XA (en) 2015-10-26 2018-05-30 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
EP4292662A3 (en) 2016-03-04 2024-02-21 Vanderbilt University Substituted indole mcl-1 inhibitors
TW201815799A (zh) 2016-07-28 2018-05-01 美商Ｔｐ生物醫藥公司 巨環激酶抑制劑
WO2018112027A1 (en) 2016-12-14 2018-06-21 Development Center For Biotechnology Antibody-drug conjugates and uses thereof
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
SI3658148T1 (sl) 2017-07-28 2024-10-30 Turning Point Therapeutics, Inc. Makrociklične spojine in njihova uporaba

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